The present invention relates to novel antitumor agents, process for their preparation, and intermediates useful therein. More particularly, the present invention relates to 10-desacetoxytaxol derivatives which are useful as intermediates in the preparation of 10-desacetoxytaxol.
Taxol is a natural product extracted from the bark of yew trees. It has been shown to have excellent antitumor activity in in vivo animal models, and recent studies have elucidated its unique mode of action, which involves abnormal polymerization of tubulin and disruption of mitosis. It is currently undergoing clinical trials against ovarian, breast and other types of cancer in the United States and France and preliminary results have confirmed it as a most promising chemotherapeutic agent. The structure of taxol and the numbering system conventionally used is shown below; this numbering system is also applicable to compounds of the present invention. ##STR1##